WEB 2086 (apafant) is a potent and selective platelet activating (PAF) antagonist. WEB 2086 has high affinity for guinea pig peritoneal macrophage PAF receptors, dissociating slowly. WEB 2086 at 10-8 to 10-6 mol/L strongly and concentration-dependently inhibits PAF-induced chemotaxis in guinea pig eosinophils. In animal models, WEB 2086 (0.1% w/v) blocks eosinophil activation in allergic conjunctivitis and inhibits the hypotensive and lethal effect of PAF in the rat in a dose-related manner.
- Pharmacological characterization of a receptor for platelet-activating factor on guinea pig peritoneal macrophages using [3H]apafant, a selective and competitive platelet-activating factor antagonist: evidence that the noncompetitive behavior of apafant in functional studies relates to slow kinetics of dissociation. Ring P. et al. Molec Pharmacol. 1993, 43, 302.
- Eosinophil chemotaxis induced by several biologically active substances and the effects of apafant on it in vitro. Nabe. Arzneimittel-Forschung 1997, 47, 1112.
- Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs. Kato M. et al. J Pharmacol Sci. 2004, 95, 435.